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Chemistry

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Also known as: Kalbitor, Fov2302, Dx-88, Gtpl6955
Molecular Formula
C305H442N88O91S8
Molecular Weight
7054  g/mol
InChI Key
VBGWSQKGUZHFPS-VGMMZINCSA-N

Ecallantide
Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in Pichia pastoris yeast cells that contains three intramolecular disulfide bonds. It was discovered by phage display technology. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI). The amino acid sequence of two compounds differ by seven amino acids. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE.
1 2D Structure

Ecallantide

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid
2.1.2 InChI
InChI=1S/C305H442N88O91S8/c1-16-152(5)241-295(478)377-195(124-168-80-82-172(398)83-81-168)252(435)334-137-227(404)333-138-228(405)345-214-143-487-491-147-218-291(474)351-179(73-47-107-327-301(315)316)255(438)341-154(7)245(428)339-155(8)249(432)379-210(127-171-136-326-150-338-171)299(482)393-113-53-79-221(393)294(477)361-181(75-49-109-329-303(319)320)260(443)372-203(125-169-134-332-175-69-40-39-68-173(169)175)277(460)370-198(119-163-58-29-20-30-59-163)274(457)369-199(120-164-60-31-21-32-61-164)275(458)375-207(130-226(314)403)284(467)389-242(153(6)17-2)296(479)378-202(123-167-66-37-24-38-67-167)283(466)390-243(159(12)396)297(480)362-182(76-50-110-330-304(321)322)258(441)353-186(86-94-223(311)400)267(450)383-217(290(473)359-188(89-98-234(414)415)263(446)354-189(90-99-235(416)417)265(448)368-201(282(465)388-241)122-166-64-35-23-36-65-166)146-490-489-145-216(384-268(451)191(92-101-237(420)421)355-262(445)187(88-97-233(412)413)357-271(454)194(116-151(3)4)366-285(468)212(141-394)381-266(449)190(91-100-236(418)419)358-273(456)197(118-162-56-27-19-28-57-162)367-259(442)180(74-48-108-328-302(317)318)349-280(463)206(129-225(313)402)374-264(447)185(85-93-222(310)399)356-279(462)205(128-224(312)401)344-229(406)139-335-251(434)184(352-288(214)471)87-96-232(410)411)289(472)350-178(72-43-46-106-308)256(439)347-177(71-42-45-105-307)257(440)360-193(103-115-486-15)270(453)385-219(292(475)391-244(160(13)397)298(481)363-183(77-51-111-331-305(323)324)261(444)380-211(300(483)484)133-240(426)427)148-492-488-144-215(386-276(459)200(121-165-62-33-22-34-63-165)371-286(469)213(142-395)382-278(461)204(126-170-135-325-149-337-170)373-269(452)192(102-114-485-14)346-246(429)156(9)340-250(433)174(309)84-95-231(408)409)287(470)343-158(11)247(430)364-196(117-161-54-25-18-26-55-161)272(455)348-176(70-41-44-104-306)254(437)342-157(10)248(431)365-209(132-239(424)425)281(464)376-208(131-238(422)423)253(436)336-140-230(407)392-112-52-78-220(392)293(476)387-218/h18-40,54-69,80-83,134-136,149-160,174,176-221,241-244,332,394-398H,16-17,41-53,70-79,84-133,137-148,306-309H2,1-15H3,(H2,310,399)(H2,311,400)(H2,312,401)(H2,313,402)(H2,314,403)(H,325,337)(H,326,338)(H,333,404)(H,334,435)(H,335,434)(H,336,436)(H,339,428)(H,340,433)(H,341,438)(H,342,437)(H,343,470)(H,344,406)(H,345,405)(H,346,429)(H,347,439)(H,348,455)(H,349,463)(H,350,472)(H,351,474)(H,352,471)(H,353,441)(H,354,446)(H,355,445)(H,356,462)(H,357,454)(H,358,456)(H,359,473)(H,360,440)(H,361,477)(H,362,480)(H,363,481)(H,364,430)(H,365,431)(H,366,468)(H,367,442)(H,368,448)(H,369,457)(H,370,460)(H,371,469)(H,372,443)(H,373,452)(H,374,447)(H,375,458)(H,376,464)(H,377,478)(H,378,479)(H,379,432)(H,380,444)(H,381,449)(H,382,461)(H,383,450)(H,384,451)(H,385,453)(H,386,459)(H,387,476)(H,388,465)(H,389,467)(H,390,466)(H,391,475)(H,408,409)(H,410,411)(H,412,413)(H,414,415)(H,416,417)(H,418,419)(H,420,421)(H,422,423)(H,424,425)(H,426,427)(H,483,484)(H4,315,316,327)(H4,317,318,328)(H4,319,320,329)(H4,321,322,330)(H4,323,324,331)/t152-,153-,154-,155-,156-,157-,158-,159-,160-,174-,176-,177-,178-,179-,180-,181-,182-,183-,184-,185-,186-,187-,188-,189-,190-,191-,192-,193-,194-,195-,196-,197-,198-,199-,200-,201-,202-,203-,204-,205-,206-,207-,208-,209-,210-,211-,212-,213-,214-,215-,216-,217-,218-,219-,220-,221-,241-,242-,243-,244-/m0/s1
2.1.3 InChI Key
VBGWSQKGUZHFPS-VGMMZINCSA-N
2.1.4 Canonical SMILES
CCC(C)C1C(=O)NC(C(=O)NCC(=O)NCC(=O)NC2CSSCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)N5CCCC5C(=O)N3)CC(=O)O)CC(=O)O)C)CCCCN)CC6=CC=CC=C6)C)NC(=O)C(CC7=CC=CC=C7)NC(=O)C(CO)NC(=O)C(CC8=CN=CN8)NC(=O)C(CCSC)NC(=O)C(C)NC(=O)C(CCC(=O)O)N)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC(=O)O)C(=O)O)CCSC)CCCCN)CCCCN)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC2=O)CCC(=O)O)CC(=O)N)CCC(=O)N)CC(=O)N)CCCNC(=N)N)CC9=CC=CC=C9)CCC(=O)O)CO)CC(C)C)CCC(=O)O)CCC(=O)O)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC1=CC=CC=C1)CCC(=O)O)CCC(=O)O)CCC(=O)N)CCCNC(=N)N)C(C)O)CC1=CC=CC=C1)C(C)CC)CC(=O)N)CC1=CC=CC=C1)CC1=CC=CC=C1)CC1=CNC2=CC=CC=C21)CCCNC(=N)N)CC1=CN=CN1)C)C)CCCNC(=N)N)CC1=CC=C(C=C1)O
2.1.5 Isomeric SMILES
CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)NCC(=O)NCC(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N4CCC[C@H]4C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N5CCC[C@H]5C(=O)N3)CC(=O)O)CC(=O)O)C)CCCCN)CC6=CC=CC=C6)C)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CN=CN8)NC(=O)[C@H](CCSC)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)N)C(=O)N[C@@H]([C@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)O)CCSC)CCCCN)CCCCN)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC2=O)CCC(=O)O)CC(=O)N)CCC(=O)N)CC(=O)N)CCCNC(=N)N)CC9=CC=CC=C9)CCC(=O)O)CO)CC(C)C)CCC(=O)O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC1=CC=CC=C1)CCC(=O)O)CCC(=O)O)CCC(=O)N)CCCNC(=N)N)[C@H](C)O)CC1=CC=CC=C1)[C@@H](C)CC)CC(=O)N)CC1=CC=CC=C1)CC1=CC=CC=C1)CC1=CNC2=CC=CC=C21)CCCNC(=N)N)CC1=CN=CN1)C)C)CCCNC(=N)N)CC1=CC=C(C=C1)O
2.2 Synonyms
2.2.1 MeSH Synonyms

1. Dx 88

2. Dx-88

3. Dx-88 Cpd

4. Epi-kal-2

5. Kalbitor

2.2.2 Depositor-Supplied Synonyms

1. Kalbitor

2. Fov2302

3. Dx-88

4. Gtpl6955

2.3 Create Date
2009-08-20
3 Chemical and Physical Properties
Molecular Weight 7054 g/mol
Molecular Formula C305H442N88O91S8
XLogP3-27.9
Hydrogen Bond Donor Count100
Hydrogen Bond Acceptor Count110
Rotatable Bond Count133
Exact Mass7052.0530407 g/mol
Monoisotopic Mass7049.0429762 g/mol
Topological Polar Surface Area3120 Ų
Heavy Atom Count492
Formal Charge0
Complexity18500
Isotope Atom Count0
Defined Atom Stereocenter Count60
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameKalbitor
PubMed HealthEcallantide (Injection)
Drug ClassesImmune Modulator
Drug LabelKALBITOR (ecallantide) is a human plasma kallikrein inhibitor for injection for subcutaneous use. Ecallantide is a 60-amino-acid protein produced in Pichia pastoris yeast cells by recombinant DNA technology.KALBITOR is a clear and colorless, sterile,...
Active IngredientEcallantide
Dosage FormInjectable
Routeinjection
Strength10mg/ml
Market StatusPrescription
CompanyDyax Corp.

2 of 2  
Drug NameKalbitor
PubMed HealthEcallantide (Injection)
Drug ClassesImmune Modulator
Drug LabelKALBITOR (ecallantide) is a human plasma kallikrein inhibitor for injection for subcutaneous use. Ecallantide is a 60-amino-acid protein produced in Pichia pastoris yeast cells by recombinant DNA technology.KALBITOR is a clear and colorless, sterile,...
Active IngredientEcallantide
Dosage FormInjectable
Routeinjection
Strength10mg/ml
Market StatusPrescription
CompanyDyax Corp.

4.2 Therapeutic Uses

Kalbitor (Ecallantide) is indicated for treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older. /Included in US product label/

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


4.3 Drug Warning

/BOXED WARNING/ WARNING: ANAPHYLAXIS. Anaphylaxis has been reported after administration of Kalbitor. Because of the risk of anaphylaxis, Kalbitor should only be administered by a healthcare professional with appropriate medical support to manage anaphylaxis and hereditary angioedema. Healthcare professionals should be aware of the similarity of symptoms between hypersensitivity reactions and hereditary angioedema and patients should be monitored closely. Do not administer Kalbitor to patients with known clinical hypersensitivity to Kalbitor.

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


Potentially serious hypersensitivity reactions, including anaphylaxis, have occurred in patients treated with Kalbitor. In 255 hereditary angioedema (HAE) patients treated with intravenous or subcutaneous Kalbitor in clinical studies, 10 patients (4%) experienced anaphylaxis. For the subgroup of 187 patients treated with subcutaneous Kalbitor, 5 patients (3%) experienced anaphylaxis. Symptoms associated with these reactions have included chest discomfort, flushing, pharyngeal edema, pruritus, rhinorrhea, sneezing, nasal congestion, throat irritation, urticaria, wheezing, and hypotension. These reactions occurred within the first hour after dosing. Other adverse reactions indicative of hypersensitivity reactions included the following: pruritus (5%), rash (3%), and urticaria (2%). Patients should be observed for an appropriate period of time after administration of Kalbitor, taking into account the time to onset of anaphylaxis seen in clinical trials. Given the similarity in hypersensitivity symptoms and acute HAE symptoms, patients should be monitored closely in the event of a hypersensitivity reaction.

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


There are no adequate and well-controlled trials of Kalbitor in pregnant women. Kalbitor has been shown to cause developmental toxicity in rats, but not rabbits. Because animal reproductive studies are not always predictive of human response, Kalbitor should be used during pregnancy only if clearly needed.

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


FDA Pregnancy Risk Category: C /RISK CANNOT BE RULED OUT. Adequate, well controlled human studies are lacking, and animal studies have shown risk to the fetus or are lacking as well. There is a chance of fetal harm if the drug is given during pregnancy; but the potential benefits may outweigh the potential risk./

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


For more Drug Warnings (Complete) data for Ecallantide (11 total), please visit the HSDB record page.


4.4 Drug Indication

Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Intravenous administration of ecallantide doses 20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG.


5.2 MeSH Pharmacological Classification

Analgesics

Compounds capable of relieving pain without the loss of CONSCIOUSNESS. (See all compounds classified as Analgesics.)


Anti-Inflammatory Agents, Non-Steroidal

Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. (See all compounds classified as Anti-Inflammatory Agents, Non-Steroidal.)


5.3 FDA Pharmacological Classification
5.3.1 Pharmacological Classes
Plasma Kallikrein Inhibitor [EPC]; Kallikrein Inhibitors [MoA]
5.4 ATC Code

B - Blood and blood forming organs

B06 - Other hematological agents

B06A - Other hematological agents

B06AC - Drugs used in hereditary angioedema

B06AC03 - Ecallantide


5.5 Absorption, Distribution and Excretion

Absorption

Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean ( standard deviation) peak plasma concentration (Cmax) of 586 106 ng/mL was achieved. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose. The mean area under the concentration-time curve (AUC) was 3017 402 ng*hr/mL.


Route of Elimination

Ecallantide undergoes renal elimination.


Volume of Distribution

The volume of distribution was 26.4 7.8 L in healthy individuals. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment.


Clearance

Plasma clearance was 153 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects. Inter-individual variability in patients and healthy individuals was 38% for clearance.


In a pharmacokinetic study in healthy individuals, peak plasma concentrations of ecallantide were achieved at approximately 2-3 hours following a 30 mg dose of ecallantide administered by subcutaneous injection; an approximate bioavailability of 90% was reported with subcutaneous administration.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3676


Ecallantide is eliminated in urine; however, since the drug is a small protein, metabolic catabolism (or degradation) is also a likely elimination process.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3676


It is not known whether ecallantide is excreted in human milk.

NIH; DailyMed. Current Medication Information for Kalbitor (Ecallantide) Injection, Solution (Revised: September 2014). Available from, as of March 24, 2015: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f56aec67-c662-477c-b866-bfc23e8809cf


5.6 Metabolism/Metabolites

Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system. No _in vitro_ metabolism studies were performed with ecallantide.


5.7 Biological Half-Life

Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 0.5 hours.


The mean half life of ecallantide is 2 hours.

American Society of Health-System Pharmacists 2015; Drug Information 2015. Bethesda, MD. 2015, p. 3676


5.8 Mechanism of Action

The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway), which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein. C1-INH inhibits both factor XIIa and kallikrein. Kallikrein may in turn reciprocally activate more FXII. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production.


Ecallantide, a biosynthetic protein based on the first Kunitz domain of human tissue factor pathway inhibitor, is a reversible and selective inhibitor of plasma kallikrein.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 3675


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01

Brand Name : Kalbitor

Ecallantide

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SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Japan
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SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Genetic Disorders

Currency : USD

2019 Revenue in Millions : 44

2018 Revenue in Millions : 0

Growth (%) : N/A

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02

Brand Name : Kalbitor

Ecallantide

arrow
SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Japan
arrow
SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Genetic Disorders

Currency : USD

2020 Revenue in Millions : 39

2019 Revenue in Millions : 45

Growth (%) : -13

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03

Brand Name : Kalbitor

Ecallantide

arrow
SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Japan
arrow
SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Genetic Disorders

Currency : USD

2021 Revenue in Millions : 34

2020 Revenue in Millions : 37

Growth (%) : -2

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04

Brand Name : Kalbitor

Ecallantide

arrow
SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Japan
arrow
SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Genetic Diseases

Currency : USD

2022 Revenue in Millions : 34

2021 Revenue in Millions : 34

Growth (%) : 0

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05

Brand Name : Kalbitor

Ecallantide

arrow
SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Japan
arrow
SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Genetic Diseases

Currency : USD

2023 Revenue in Millions : 0

2022 Revenue in Millions : 34

Growth (%) : -100

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06

Brand Name : Kalbitor

Ecallantide

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SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Ireland
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SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Dermatology

Currency : USD

2016 Revenue in Millions : 52

2015 Revenue in Millions : Not Reported

Growth (%) : Not Reported

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07

Brand Name : Kalbitor

Ecallantide

arrow
SupplySide West 2024
Not Confirmed

Brand Name : Kalbitor

Ireland
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SupplySide West 2024
Not Confirmed

Ecallantide

Main Therapeutic Indication : Dermatology

Currency : USD

2017 Revenue in Millions : 67

2016 Revenue in Millions : 52

Growth (%) : 29

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